Pronunciation: CAR-tee-oh-lahl HIGH-droe-KLOR-ide
Class: Beta-adrenergic blocking agent
- Tablets 2.5 mg
- Tablets 5 mg
- Solution, ophthalmic 1%
Blocks beta-receptors, primarily affecting cardiovascular system (eg, decreases heart rate, cardiac contractility, BP) and lungs (promotes bronchospasm). Ophthalmic use reduces IOP, probably by decreasing aqueous production.
Well absorbed. T max is 1 to 3 h. Bioavailability is about 85%.
23% to 30% protein bound.
Metabolized to 8-hydroxycarteolol (active) and glucuronide conjugates.
The t ½ is about 6 h (carteolol) and about 8 to 12 h (8-hydroxycarteolol). About 50% to 70% is excreted unchanged by the kidneys.
Special PopulationsRenal Function Impairment
The t ½ may be prolonged and elimination decreased. Dosage adjustment may be needed.
Indications and Usage
Management of hypertension. Ophthalmic preparation for control of intraocular hypertension and lowering of IOP in chronic open-angle glaucoma.
Treatment of angina.
Hypersensitivity to beta-blockers; persistently severe bradycardia; greater than first-degree AV block; CHF unless secondary to tachyarrhythmia treatable with beta-blockers; overt cardiac failure; sinus bradycardia; cardiogenic shock; bronchial asthma or bronchospasm, including severe chronic obstructive pulmonary disease (COPD).
Dosage and AdministrationAdults
PO 2.5 to 10 mg every day.Ophthalmic use
1 drop twice daily in affected eye(s). Consider concomitant therapy if IOP is not at satisfactory level.
For ophthalmic solution, pull out lower lid to create pocket, administer drop without touching eye, release lower lid, close eye, and apply gentle pressure on inner canthus of eye to avoid systemic absorption.
Store at room temperature.
May enhance or reverse antihypertensive effect; may cause potentially life-threatening increases in BP, especially on simultaneous discontinuation of both drugs.Epinephrine
May cause initial hypertensive episode followed by bradycardia.Ergot derivatives
May cause peripheral ischemia with cold extremities. Peripheral gangrene possible.NSAIDs
May impair antihypertensive effect.Prazosin
May increase orthostatic hypotension.Systemic beta-blocker
When coadministered with ophthalmic carteolol hydrochloride solution, may cause additive effects and toxicity.Theophyllines
May reduce elimination of theophylline. May cause pharmacologic antagonism, reducing effects of one or both drugs.Verapamil
May increase effects of both drugs.
Laboratory Test Interactions
None well documented.
Hypotension; bradycardia; CHF; cold extremities; first-, second-, or third-degree atrioventricular block; arrhythmias; syncope.
Insomnia; fatigue; dizziness; depression; lethargy; drowsiness; forgetfulness; headache.
Rash; hives; alopecia.
Dry eyes; blurred vision; tinnitus; slurred speech; dry mouth; sore throat. Eye discomfort or stinging; tearing; keratitis; drooping eyelids; visual disturbances; diplopia; ptosis (ophthalmic use).
Nausea; vomiting; diarrhea; constipation.
Impotence; painful, difficult, or frequent urination.
Agranulocytosis; thrombocytopenic purpura.
Hyperglycemia; hypoglycemia; unstable diabetes mellitus; hypercholesterolemia; hyperlipidemia; increased LDH.
Bronchospasm; shortness of breath; wheezing.
Weight changes; fever; facial swelling; cramps; muscle weakness. Antinuclear antibodies may develop.
Monitor BP and pulse frequently when starting oral medication or when dosage is changed.IOP
Perform measurements of IOP on regular basis to assess therapeutic effect of ophthalmic medication.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
Requires dosage adjustment.
Requires dosage adjustment.
Cessation of therapy
Discontinue therapy gradually, over about 2 wk, with careful observation of patient and limited physical activity.
Administer cautiously in patients with CHF treated with digitalis and diuretics.
Drug may mask signs and symptoms of hypoglycemia (eg, tachycardia, BP changes). May potentiate insulin-induced hypoglycemia.
Peripheral vascular disease
Drug may precipitate or aggravate symptoms of arterial insufficiency.
May mask clinical signs of developing or continuing hyperthyroidism (eg, tachycardia). Abrupt withdrawal may exacerbate symptoms of hyperthyroidism, including thyroid storm.
Bradycardia, cardiac failure, hypotension, bronchospasm, hypoglycemia.
- Instruct patient in proper method of instilling eye drops.
- Teach patient how to monitor pulse before taking oral medication and to notify health care provider if pulse remains less than 50 bpm after taking drug and if fatigue and dizziness occur.
- Instruct patient to inform health care provider of any scheduled surgery or dental work; dosage may need to be gradually tapered (and ophthalmic solution discontinued) before surgery or treatment.
- Caution patient not to discontinue medication without consulting health care provider.
- Instruct diabetic patient to monitor blood glucose closely because carteolol hydrochloride may mask signs of hypoglycemia.
- Inform patient that ophthalmic solution may cause burning or stinging when first instilled in eye.
- Instruct patient to report these symptoms to health care provider: CHF, dizziness, decreased pulse, confusion, shortness of breath, rash, any unusual bleeding.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
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